ANALGESIC AND ANTI INFLAMMATORY ACTIVITY OF NEW SUBSTITUTED THIAZOLIDIN-4-ONE DERIVATIVES
Journal: Indo American Journal of Pharmaceutical Sciences (IAJPS) (Vol.04, No. 08)Publication Date: 2017-08-17
Authors : Dr.Faizan Sayeed; Abdul Sayeed; MD Akram; Mohd Waseem Akram;
Page : 2449-2460
Keywords : Schiffbases; Thiazolidin-4-one; Analgesic; Anti- inflammatory;
Abstract
4-thiazolidinones are among t h e most extensively investigated class of organic compounds. Thiazolidin-4-one has been considered as magic moiety, which is a core structure in various synthetic pharmaceuticals displaying a broad spectrum of biological activities.They are widely used as anti-inflammatory, anticonvulsant, analgesic, antimicrobial,anti-HIV,CNS depressant, carcinostatic, antihypertensive and cytotoxic. In view of the wide spectrum activities of condensed 4-thiazolidinones, itwas thought worthwhile to undertake the synthesis of heterocyclic systems in which 4-thiazolidinone nucleus is linked to another biologically active moiety.Semicarbazide/Thiosemicarbazide was reacted with b e n z o y l chloride to obtain N-hydrazinocarbonyl benzene-1-carboxamide/N-hydrazinocarbothioyl benzene-1 carboxamide respectively.These were then condensed with various aldehydes to yield the intermediate Schiff bases. Thiazolidin-4-ones were prepared by the reaction of Schiff bases with mercaptoacetic acid in dry benzene by refluxing for 16-18 hours. The purity of the compounds synthesized was established by TLC.The synthesized derivatives were characterized by FT-IR, 1 HNMR and Mass spectral analysis. All the derivatives synthesized were screened for their a n a lg e s i c a n d a n t i in f l a m ma t o r y potency. The compounds 3A3, 3A5,3B2, 3B6 have shown equipotent analgesic activity when compared to standard Ibuprofen. The compounds 3A2, 3A5, 3B2, and 3B3 have been evaluated for their antiinflammatory properties at a dose of 50 mg/kg using carrageenan induced rat paw edema method. All the tested compounds exhibited significant anti-inflammatory activity in acute inflammatory models in rats.Compounds 3A2, 3A5, 3B2, and 3B3 exhibited s i g n i f i c a n t r e d u c t i o n i n e d e m a volume w h e n c o m p a r e d t o s t a n d a r d Ibuprofen. Keywords: Schiffbases,Thiazolidin-4-one,Analgesic,Anti- inflammatory
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